Plural Nitrogens In Acid Moiety Patents (Class 560/13)
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Patent number: 6767922Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: September 6, 2002Date of Patent: July 27, 2004Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Qi Jin
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Patent number: 6747148Abstract: Sulfonamide derivatives, their physiologically tolerable salts and their prodrugs according to the present invention are vitronectin receptor antagonists and inhibitors of cell adhesion, as well as inhibit bone resorption by osteoclasts. These derivatives, salts and prodrugs are pharmaceutically active compounds useful in the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. Processes for the preparation of the sulfonamide derivatives according to the present invention, the use of these derivatives as pharmaceutically active ingredients, and pharmaceutical preparations comprising these derivatives also are disclosed.Type: GrantFiled: October 9, 2001Date of Patent: June 8, 2004Assignees: Hoechst Marion Roussel Deutschland GmbH, Genentech, Inc.Inventors: Anuschirwan Peyman, David William Will, Jochen Knolle, Karlheinz Scheunemann, Denis Carniato, Jean-Francois Gourvest, Thomas R. Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
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Patent number: 6743929Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 6, 2000Date of Patent: June 1, 2004Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 6727282Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 9, 2002Date of Patent: April 27, 2004Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Publication number: 20040034070Abstract: The invention relates to phenoxypropanolamines, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of diseases that are improved by beta-3 agonist action.Type: ApplicationFiled: August 8, 2003Publication date: February 19, 2004Inventors: Laura Barzaghi, Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Stefano Romagnano
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Patent number: 6693137Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: January 23, 2001Date of Patent: February 17, 2004Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, David Michael Bender, Buddy Eugene Cantrell, Winton Dennis Jones, Paul Leslie Ornstein, Richard Lee Simon, Edward C. R. Smith, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6683210Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: March 15, 2002Date of Patent: January 27, 2004Assignee: G. D. Searle & Co.Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Patent number: 6677360Abstract: The present invention relates to biphenyl and biphenyl-analogous compounds, their preparation and use as pharmaceutical compositions, as integrin antagonists and in particular for the production of pharmaceutical compositions for the treatment and prophylaxis of cancer, arteriosclerosis, restenosis, osteolytic disorders such as osteoporosis and ophthalmic diseases. The compounds according to the invention have the formula (1) wherein R1, R2, U, V, A, B, W, R3, C and R4 have the meaning as defined in the claims.Type: GrantFiled: April 6, 2001Date of Patent: January 13, 2004Assignee: Bayer AktiengesellschaftInventors: Markus Albers, Klaus Urbahns, Andrea Vaupel, Michael Härter, Delf Schmidt, Beatrix Stelte-Ludwig, Christoph Gerdes, Elke Stahl, Jörg Keldenich, Ulf Brueggemeier, Klemens Lustig
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Patent number: 6667414Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: November 28, 2001Date of Patent: December 23, 2003Assignee: Pharmacia CorporationInventors: Gunnar J. Hanson, John S. Baran
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Publication number: 20030229228Abstract: The invention relates to novel pesticidally active &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1-R9 have the meanings given in the specification R10 is either hydrogen, (a), (b), (c), (d) or (e) wherein R13, R14, R16, R17 and R19 are each independently hydrogen or C1-C4 alkyl, R15 is C4-C12 alkyl; C1-C12 halogenalkyl; C3-C8 cycloalkyl; optionally substituted aryl or optionally substituted heteroaryl, R18 is optionally substituted aryl or optionally substituted heteroaryl; and Z is oxygen, sulfur —CR20R21— or —NR22—, wherein R20, R21 and R22 independently of each other are hydrogen of C1-C4 alkyl; provided that when R8 is hydrogen, R9 is not C1-C6-alkoxy, C3-C6 alkenyloxy or C3-C6-alkynyloxy in position 3 of the phenyl ring carrying these radicals.Type: ApplicationFiled: February 20, 2003Publication date: December 11, 2003Inventors: Martin Zeller, Clemens Lamberth, Henry Szczepanski, Alain De Mesmaeker
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Publication number: 20030216375Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: September 17, 2002Publication date: November 20, 2003Inventors: Michael R. Palovich, Katherine L. Widdowson, Hong Nie
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Publication number: 20030208087Abstract: The present invention relates to a compound of the formula (I) 1Type: ApplicationFiled: March 13, 2003Publication date: November 6, 2003Inventors: Klaus Lorenz, Hans-Joachim Ressel, Lothar Willms
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Patent number: 6632816Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, wherein R1 may be, for example, iso-butyl, wherein X and Y, same or different, may be, for example, NH2 and F, and wherein R2 and R3 are as defined herein.Type: GrantFiled: December 23, 2002Date of Patent: October 14, 2003Assignee: Pharmacor Inc.Inventors: Brent Richard Stranix, Jean-François Lavallée, Nicolas LeBerre, Valérie Perron
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Publication number: 20030187065Abstract: The present invention relates to 1-(aryloxy)propionoyl-2-arylsulfonyl hydrazines useful as hypoglycemic agents, and to a process for synthesis thereof. The present invention also relates to the synthesis of 1-(aryloxy)propionoyl-2-arylsulfonyl hydrazines as new hypoglycemic agents which may be useful in the treatment of diabetes.Type: ApplicationFiled: March 29, 2002Publication date: October 2, 2003Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Ramalingam Thallapalli, Venkata Durga Nageswar Yadavalli, Ramakrishna Sistla, Adari Bhaskar Rao, Prakash Vamanrao Diwan, Jhillu Singh Yadav, Kondapuram Vijaya Raghavan
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Patent number: 6620933Abstract: A azomethine yellow dye compound of general formula (I): General formula (I) wherein R1 and R2 each independently represent a hydrogen atom or a substituent; R3 represents a substituent; m indicates an integer from 0 to 3; when m is 2 or greater, R3's may be the same or different and may be mutually bonded to form a condensed ring; R3 may be bonded to R1 or R2 to form a condensed ring; R4 represents an aryl group or a heterocyclic group; R5 and R6 each independently represent a hydrogen atom or a substituent; R7 represents a substituent; n indicates an integer from 0 to 4; when n is 2 or greater, R7's may be the same or different and the may be mutually bonded to form a condensed ring; R7 may be bonded to R5 or R6 to form a condensed ring; and R5 and R6 may be bonded to each other to form a ring.Type: GrantFiled: September 26, 2002Date of Patent: September 16, 2003Assignee: Fuji Photo Film Co., Ltd.Inventors: Kiyoshi Takeuchi, Shigeki Uehira
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Publication number: 20030166685Abstract: Compounds having the formula (I), 1Type: ApplicationFiled: November 7, 2001Publication date: September 4, 2003Inventors: Gregory S. Bisacchi, James C. Sutton, William A. Slusarchyk, Uwe D. Treuner, Guohua Zhao, Daniel L. Cheney, Yan Shi, Shung C. Wu
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Patent number: 6603044Abstract: The present invention provides a phthalamide derivative of the formula (I): wherein A1 is (substituted) C1-C8 alkylene, (substituted) C3-C8 alkenylene, (substituted) C3-C8 alkynylene, etc., R1 is H, (halo) C3-C6 cycloalkyl, (substituted) phenyl, (substituted) heterocycle, —A2—R4, etc., R2 and R3 are H, C3-C6 cycloalkyl, —A2—R4, etc., A2 is —C(═O)—, —C(═S)— or —C(═NR5)—, R4 is H, alkyl, (substituted) phenyl, (substituted) heterocycle, etc., X and Y are halogen, cyano, nitro, (halo) C1-C6 alkyl, (halo) C1-C6 alkoxy, etc., l is 0-4, m is 0-5, n is 0-2; and an agrohorticultural insecticide containing said compound as active ingredient and exhibiting an excellent insecticidal effect.Type: GrantFiled: November 29, 1999Date of Patent: August 5, 2003Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masanori Tohnishi, Hayami Nakao, Eiji Kohno, Tateki Nishida, Takashi Furuya, Toshiaki Shimizu, Akira Seo, Kazuyuki Sakata, Shinsuke Fujioka, Hideo Kanno
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Publication number: 20030138712Abstract: An organophotoreceptor that includes:Type: ApplicationFiled: November 6, 2002Publication date: July 24, 2003Applicant: SAMSUNG Electronics Co. Ltd.Inventors: Kam W. Law, Nusrallah Jubran, Zbigniew Tokarski, Alan R. Katrizky, Ritu Jain, Anatoliy Vakulenko
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Patent number: 6583180Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are novel glucocorticoid receptor modulators and are useful for treating type II diabetes in a mammal.Type: GrantFiled: February 8, 2002Date of Patent: June 24, 2003Assignee: Abbott LaboratoriesInventors: James T. Link, Bryan K. Sorensen, Jyoti R. Patel, David L. Arendsen, Gaoquan Li
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Patent number: 6562842Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: May 30, 2002Date of Patent: May 13, 2003Assignee: SmithKline Beecham CorporationInventor: Dennis Shinji Yamashita
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Publication number: 20030083504Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: 1Type: ApplicationFiled: October 4, 2002Publication date: May 1, 2003Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
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Publication number: 20030078284Abstract: The subject invention provides compounds which are easily metabolized by the metobolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.Type: ApplicationFiled: October 18, 2002Publication date: April 24, 2003Inventor: Pascal Druzgala
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Patent number: 6552079Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian integrins are disclosed. The compounds are useful in vitro or in vivo for preventing or treating thrombotic or restenotic disorders.Type: GrantFiled: May 15, 2001Date of Patent: April 22, 2003Assignee: Eli Lilly and CompanyInventors: Robert M. Scarborough, Mark Smyth, Ting Su, Matthew J. Fisher, Joseph A. Jakubowski, John J. Masters, Jeffry Bernard Franciskovich
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Patent number: 6552082Abstract: A solution of N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetra-hydrate (I) comprising at least one pH adjuster selected from tri-sodium phosphate, a hydrate thereof, sodium hydroxide or potassium hydroxide and a drug product using the solution. According to the invention, the solubility of the compound (I) increases and thereby it is possible to provide a solution thereof and a drug product using it. Moreover, by using a mixture of water and an organic solvent, greatly improved solubility makes it possible to manufacture a solution of higher concentration of the compound (I), and high-dosage drug products using it.Type: GrantFiled: June 18, 2001Date of Patent: April 22, 2003Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Akira Takada, Masao Sudoh
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Publication number: 20030065188Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: September 6, 2002Publication date: April 3, 2003Inventors: Katherine Louisa Widdowson, Qi Jin
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Patent number: 6538150Abstract: The present invention relates to a compound of the formula (I) The compound according to the invention is suitable for the preparation of herbicidal active substances such as sulfonylureas.Type: GrantFiled: July 20, 2001Date of Patent: March 25, 2003Assignee: Aventis CropScience GmbHInventors: Klaus Lorenz, Hans-Joachim Ressel, Lothar Willms
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Patent number: 6534495Abstract: The invention relates to a compound having the formula (I): R1SO2—B—X—Z—C(O)—Y, B is a bond, an amino acid of the formula —NR—CH[(CH2)pC(O)OH]—C(O)— or an ester derivative thereof wherein p is 1, 2, or 3, Gly, D-1-Piq, D-3-Piq, D-1-Tiq, D-3-Tiq, D-Atc, Aic, or a L- or D-amino acid having a hydrophobic, basic or neutral side chain; X is an amino acid with a hydrophobic side chain, glutamine, serine, theronine, a cyclic amino acid optionally containing an additional heteroatom selected from N, O or S, and optionally substituted with (1-6C)alkyl, (1-6C)alkoxy, benzyloxy or oxo, or X is 2-amino-isobutyric acid, —NR2—CH2—C(O)— or the fragment (I) or (II), wherein n is 2, 3, or 4, W is CH or N and R3 is H, (1-6C)alkyl or phenyl which groups may optionally be substituted with hydroxy, (1-6C)alkoxy, COOH, COO(1-6C)alkyl, CONH2, or halogen; Z is lysine or 4-aminocyclohexylglycine.Type: GrantFiled: October 26, 1999Date of Patent: March 18, 2003Assignee: Akzo NebelInventor: Anton Egbert Peter Adang
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Patent number: 6528532Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula: and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, Y is O, S, NH or N—CN, wherein Cx may be, for example COOH, or CH2OH, wherein R1 is selected from the group consisting of a benzenesulfonyl group of formula II as defined herein, wherein R2 may be, for example, iso-butyl, or 3-methylbutyl, and wherein R3 and R4 are as defined herein.Type: GrantFiled: May 13, 2002Date of Patent: March 4, 2003Assignee: Pharmacor Inc.Inventors: Brent Richard Stranix, Abderrahim Bouzide, Gilles Sauvé
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Patent number: 6528543Abstract: Glucokinase activating compounds of the formula wherein R1 and R2 are independently hydrogen, halo, amino, nitro, cyano, sulfonamido, lower alkyl, perfluoro-lower alkyl, lower alkyl thio, perfluoro-lower alkyl thio, lower alkyl sulfonyl, or perfluoro-lower alkyl sulfonyl; R3 is cycloalkyl having from 3 to 7 carbon atoms or lower alkyl having from 2 to 4 carbon atoms; R4 is hydrogen, lower alkyl, lower alkenyl, hydroxy lower alkyl, halo lower alkyl, R5 and R6 are hydrogen or lower alkyl; and n is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt thereofType: GrantFiled: March 21, 2000Date of Patent: March 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Fred Thomas Bizzarro, Wendy Lea Corbett, Antonio Focella, Joseph Francis Grippo, Nancy-Ellen Haynes, George William Holland, Robert Francis Kester, Paige Erin Mahaney, Ramakanth Sarabu
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Patent number: 6515024Abstract: Succinoylamino hydroxyethylamino sulfonyl urea derivatives are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: December 11, 2001Date of Patent: February 4, 2003Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 6500832Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 14, 2000Date of Patent: December 31, 2002Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Patent number: 6498253Abstract: Compounds of the formula (I) and salts thereof in which W1, W2, R, n, R1, R2, R4, X, Y and Z are as defined in claim 1 and R3 is an acyl radical, are suitable as herbicides and plant growth regulators. The herbicides can be prepared by the process variants from claim 5, the novel intermediate products (II), (IV), (VI) and (VIII)* of claims 9 and 10 being employed.Type: GrantFiled: February 25, 1999Date of Patent: December 24, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Patent number: 6495604Abstract: The present invention provides a compound represented by the formula: wherein R represents an aliphatic hydrocarbon group optionally having substituents, an aromatic hydrocarbon group optionally having substituents, a heterocyclic group optionally having substituents, a group represented by the formula: OR1 (wherein R1 represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents) or a group represented by the formula: wherein R1b represents a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R1c is, same with or different from R1b, a hydrogen atom or an aliphatic hydrocarbon group optionally having substituents, R0 represents a hydrogen atom or an aliphatic hydrocarbon group, or R and R0 represents a bond with each other, Ar represents an aromatic hydrocarbon group optionally having substituents, and n is an integer of 1 to 4, or a salt thereof, which is a agent for preventing or treating diseaseType: GrantFiled: August 14, 2000Date of Patent: December 17, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Yuzo Ichimori, Masayuki Ii, Katsumi Itoh, Tomoyuki Kitazaki, Junji Yamada
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Patent number: 6492421Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: July 30, 1998Date of Patent: December 10, 2002Assignees: Athena Neurosciences, Inc., American Home Products Corp.Inventors: Eugene D. Thorsett, Christopher M. Semko, Dimitrios Sarantakis, Michael A. Pleiss, Louis John Lombardo, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Michael S. Dappen, Reinhardt Bernhard Baudy, Susan Ashwell
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Patent number: 6482849Abstract: The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of &agr;4&bgr;1 mediated adhesion to either VCAM or CS-1 and which can be used for treating or preventing &agr;4&bgr;1 adhesion mediated conditions in a mammal such as a human.Type: GrantFiled: June 23, 1998Date of Patent: November 19, 2002Assignees: Tanabe Seiyaku Co., Ltd., Pharmacia & Upjohn CompanyInventors: Thomas J. Lobl, Bradley R. Teegarden, Alexander Polinsky, Gilbert M. Rishton, Masafumi Yamagishi, Steven Tanis, Jed F. Fisher, Edward W. Thomas, Robert A. Chrusciel
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Patent number: 6476027Abstract: An N-hydroxy sulfonyl butanamide compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated N-hydroxy sulfonyl butanamide compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: December 6, 1999Date of Patent: November 5, 2002Assignee: Monsanto CompanyInventors: Clara I. Villamil, John N. Freskos, Brent V. Mischke, Patrick B. Mullins, Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Thomas E. Barta, Daniel P. Becker
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Patent number: 6472393Abstract: Compounds having the structure shown below wherein A, B, N1, N2, X, Y, Q, R2, R5 and R6 are as defined herein are useful to inhibit serine protease enzymes, such as TF/factor VIIa factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: March 21, 2000Date of Patent: October 29, 2002Assignee: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, Dean R. Artis, Michael S. Dina, John A. Flygare, Richard A. Goldsmith, Regina A. Munroe, Alan G. Olivero, Richard Pastor, Thomas E. Rawson, Kirk D. Robarge, Daniel P. Sutherlin, Kenneth J. Weese, Aihe Zhou, Yan Zhu
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Patent number: 6469207Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 20, 2001Date of Patent: October 22, 2002Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Publication number: 20020137742Abstract: Compound of formula (I): 1Type: ApplicationFiled: March 14, 2002Publication date: September 26, 2002Inventors: Gilbert Lavielle, Bernard Cimetiere, Tony Verbeuren, Serge Simonet, Jean-Jacques Descombes
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Patent number: 6455587Abstract: The present invention relates to a class of amino acid derivatives with HIV aspartyl protease inhibitory properties.Type: GrantFiled: March 15, 2000Date of Patent: September 24, 2002Assignee: Pharmacor Inc.Inventors: Abderrahim Bouzide, Gilles Sauvé, Brent Richard Stranix, Guy Sévigny, Jocelyn Yelle
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Patent number: 6451791Abstract: An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a contemplated amidoaromatic ring sulfonamide hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: September 17, 2002Assignee: Monsanto CompanyInventors: Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard, S. Zaheer Abbas
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Patent number: 6448290Abstract: The sulfonamide or carboamide derivatives of the formula (I) and a pharmaceutical composition which comprise them as an active ingredient: (wherein A ring, B ring is carbocyclic ring, heterocyclic ring; Z1 is —COR1, —CH═CH—COR1 etc.; Z2 is H, alkyl etc.; Z3 is single bond, alkylene; Z4 is SO2, CO; Z5 is alkyl, phenyl, heterocyclic ring etc.; R2 is CONR8, O, S, NZ6, Z7-alkylene, alkylene etc.; R3 is H, alkyl, halogen, CF3 etc.; R4 is H, (substituted) alkyl etc.; n, t is 1-4). The compounds of the formula (I) can bind to receptors of PGE2 and show antagonistic activity against the action thereof or agonistic activity. Therefore, they are considered to be useful as medicine for inhibition of uterine contraction, analgesics, antidiarrheals, sleep inducers, medicine for increase of vesical capacity or medicine for uterine contraction, cathartic, suppression of gastric acid secretion, antihypertensive or diuretic agents.Type: GrantFiled: June 18, 1999Date of Patent: September 10, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Yuuki Nagao
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Publication number: 20020123494Abstract: One embodiment of the present invention relates to acylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), 1Type: ApplicationFiled: November 2, 2001Publication date: September 5, 2002Inventors: Holger Heitsch, Heinrich Christian Englert
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Patent number: 6433017Abstract: In accordance with the present invention, there are provided amphiphilic polyamine compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: February 28, 2001Date of Patent: August 13, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
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Patent number: 6420603Abstract: A novel process for the preparation of N,N′-bis[2,3-dihydroxypropyl]-5-[(hydroxyacetyl) methylamino]-2,4,6-triiodo-1, 3-benzenedi carboxamide of formula (I), commonly known as lomeprol, a novel non-ionic contrast agent which shows very good safety and contrast effectiveness.Type: GrantFiled: July 17, 2001Date of Patent: July 16, 2002Assignee: Bracco International B.V.Inventors: Laura Alessandroni, Patrizia Ambrosetti, Maria Argese, Renato Geremia, Enrico Moretti, Vittorio Valle, Giorgio Ripa, Marcella Murru
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Patent number: 6417387Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 5, 2001Date of Patent: July 9, 2002Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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Publication number: 20020077357Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.Type: ApplicationFiled: October 4, 2001Publication date: June 20, 2002Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
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Patent number: 6403644Abstract: The present invention is related to: (i) matrix metalloproteinase inhibitors containing sulfonylamino acid derivatives of the formula (Ia); wherein R1 is hydrogen, C1-4 alkyl; R2 is hydrogen, C1-8 alkyl etc.; E is —CONR3—, in which R3 is hydrogen, C1-4 alkyl etc., —NR3CO—, —CO—O—, —O—CO— etc.; A is hydrogen, C1-8 alkyl, C3-7 cycloalkyl, or Ar; J is bond, C2-4 alkylene etc.; G is — (CH2)m—, in which m is 2, 3 or 4, or in which R6 and R7 is hydrogen, C1-8 alkyl etc.; and non-toxic salts thereof, (ii) sulfonylamino acid derivatives of the formula (Ib): wherein all the symbols are the same meaning as (i); and non-toxic salts thereof, and (iii) process for the preparation of the compound of the formula (Ib). The compounds of the formula (Ia) are useful for prevention and/or treatment of diseases induced by overexpression and excess activity of MMP.Type: GrantFiled: November 13, 2000Date of Patent: June 11, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhito Sakaki, Hidekazu Kanazawa, Tsuneyuki Sugiura, Tohru Miyazaki, Hiroyukii Ohno
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Publication number: 20020065271Abstract: Sulfonamide derivatives, their physiologically tolerable salts and their prodrugs according to the present invention are vitronectin receptor antagonists and inhibitors of cell adhesion, as well as inhibit bone resorption by osteoclasts. These derivatives, salts and prodrugs are pharmaceutically active compounds useful in the therapy and prophylaxis of diseases which are caused at least partially by an undesired extent of bone resorption, for example of osteoporosis. Processes for the preparation of the sulfonamide derivatives according to the present invention, the use of these derivatives as pharmaceutically active ingredients, and pharmaceutical preparations comprising these derivatives also are disclosed.Type: ApplicationFiled: October 9, 2001Publication date: May 30, 2002Inventors: Anuschirwan Peyman, David William Will, Jochen Knolle, Karlheinz Scheunemann, Denis Carniato, Jean-Francois Gourvest, Thomas R. Gadek, Robert Mcdowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson
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Patent number: 6391918Abstract: Novel &agr;-amino acid amides of formula (I) as well as possible isomers and mixtures of isomers thereof, wherein the substituents are defined as follows: n is the number zero or one; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; or a group NRaRb wherein Ra and Rb are each independently of the other hydrogen, alkyl or form together an alkylene bridge; R2 is hydrogen or alkyl; R3 is optionally substituted aryl or heteroaryl; A is alkylene; and B is optionally substituted aryl; with the exception of the following compounds 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methylphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-chlorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-nitrolphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methoxyphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-fluorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-phenyl-sulfonylamino-acetamide and 2-phenyl-N-(1-pType: GrantFiled: August 25, 2000Date of Patent: May 21, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: André Jeanguenat, Martin Zeller